发明名称 |
HETEROCYCLIC SELF-IMMOLATIVE LINKERS AND CONJUGATES |
摘要 |
The present invention provides heterocyclic linker compounds useful for linking drug moieties to ligands. The compounds also include drug-ligand conjugates comprising a ligand capable of targeting a selected cell population, and a drug connected to the ligand by a heterocyclic linker moiety. The linker moiety comprises a peptide sequence that is a substrate for an intracellular enzyme, for example a cathepsin, that cleaves the peptide at an amide bond. The peptide further contains a self-immolating moiety which connects the drug and the protein peptide sequence. Upon cleavage of the peptide sequence by an intracellular enzyme the self-immolating moiety cleaves itself from the drug moiety such that the drug moiety is in an underivatized and active form. |
申请公布号 |
EP1718667(A2) |
申请公布日期 |
2006.11.08 |
申请号 |
EP20050714044 |
申请日期 |
2005.02.22 |
申请人 |
GENENTECH, INC.;SEATTLE GENETICS, INC. |
发明人 |
FENG, BAINIAN |
分类号 |
C07K5/062;A01N57/00;A61K31/427;A61K38/04;A61K38/05;A61K38/06;A61K38/17;A61K38/18;A61K38/20;A61K38/28;A61K38/30;A61K47/48;A61P35/00;C07D277/46;C07D417/02;C07D417/12;C07K1/00;C07K5/06 |
主分类号 |
C07K5/062 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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